期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 13, 页码 3871-3876出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.041
关键词
Sodium channel blockers; Na(V)1.7 blocker; Neuropathic pain; Phenyl isoxazoles; Voltage-gated channel
Blocking of certain sodium channels is considered to be an attractive mechanism to treat chronic pain conditions. Phenyl isoxazole carbamate 1 was identified as a potent and selective Na(V)1.7 blocker. Structural analogues of 1, both carbamates, ureas and amides, were proven to be useful in establishing the structure-activity relationship and improving ADME related properties. Amide 24 showed a good overall in vitro profile, that translated well to rat in vivo PK. (C) 2011 Elsevier Ltd. All rights reserved.
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